Novel inhibitors of the EGFR kinase targeting the asymmetric activating dimer interface

a dimer and inhibitor technology, applied in the field of molecular biology, biochemistry and cell biology of the epidermal growth factor receptor (egfr), can solve the problems of ineffective pharmaceuticals for many egfr-related illnesses, inefficient process for most drug discovery uses, and interference of egfr kinase activity of these proteins
US20100120678A1Inactive Publication Date: 2010-05-13RGT UNIV OF CALIFORNIA
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Patent Information

Authority / Receiving Office
US · United States
Current Assignee / Owner
RGT UNIV OF CALIFORNIA
Publication Date
2010-05-13
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides methods and compositions for the modulation of EGFR activity, in particular, inhibition of EGFR activation through an allosteric mechanism is discloses, as is a method for targeted drug discovery and design based on models of the three dimensional structure of the kinase domains of the protein dimers.
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Description

CROSS-REFERENCE TO RELATED APPLICATIONS

[0001] The present application claims the benefit of the filing dates of U.S. Provisional Patent Application No. 60 / 851,668, filed Oct. 13, 2006, and of U.S. Provisional Patent Application No. 60 / 851,921, filed Oct. 13, 2006, which are both incorporated by reference in their entirety for all purposes.FIELD OF THE INVENTION

[0002] The invention relates generally to the field of molecular biology, biochemistry, and cell biology of the Epidermal Growth Factor Receptor (EGFR). In particular, the instant invention provides methods and compositions for the modulation of EGFR. EGFR receptors play critical roles in regulating cell proliferation, differentiation, and migration, and their abnormal activation is associated with a variety of human cancers, including lung, breast, pancreatic, ovarian and prostate cancer. Compositions and methods of the invention can be used to prevent, cure, treat, or ameliorate these cancers as well as other diseases associat...

Claims

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